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![Process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3h]indol]-2′[1′H]one derivatives](/abs-image/US/2003/04/01/US06541643B1/abs.jpg.150x150.jpg)
1.发明授权Process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3h]indol]-2′[1′H]one derivatives 失效螺[顺-4-（β-羟乙氧基）环己烷 - [3h]吲哚] -2'[1'H]一种衍生物的制备方法公开(公告)号：US06541643B1
公开(公告)日：2003-04-01
申请号：US10030649
申请日：2002-04-17
申请人： Gergely Héja , Éva Csikós , Csaba Gönczi , Judit Halász , Félix Hajdú , István Hermecz , László Kis , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
发明人： Gergely Héja , Éva Csikós , Csaba Gönczi , Judit Halász , Félix Hajdú , István Hermecz , László Kis , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07D20996
CPC分类号： C07D209/96
摘要： The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.
摘要翻译： 本发明涉及制备式（I）的螺[顺-4-（β-羟乙氧基）环己烷 - [3 H]吲哚] -2'[1'H] - 酮衍生物的方法，其中R 1和R 2是 通过还原一般的[（1,3-二氧戊环）-2,4'-环己烷-1,3' - [3 H]吲哚] -2“[1'H] - 酮衍生物 式（II）其中R1和R2如本文所定义，其包括在路易斯酸存在下用氰基硼氢化钠进行还原（a），或（b）在强酸存在下用硼氢化钠进行还原（a）。
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![PROCESS FOR THE PREPARATION OF N-(1,1-DIMETHYLETHYL)-4-[[5′-ETHOXY-4-CIS[2-(4-MORPHOLINO)ETHOXY]-2′-OXOSPIRO[CYCLOHEXAN-1,3′[H]INDOL]1′(2′-H)-YL]-SULFONYL]-3-METHOXYBENZAMIDE AND ITS SALTS](/abs-image/US/2003/07/29/US06600039B1/abs.jpg.150x150.jpg)
2.发明授权PROCESS FOR THE PREPARATION OF N-(1,1-DIMETHYLETHYL)-4-[[5′-ETHOXY-4-CIS[2-(4-MORPHOLINO)ETHOXY]-2′-OXOSPIRO[CYCLOHEXAN-1,3′[H]INDOL]1′(2′-H)-YL]-SULFONYL]-3-METHOXYBENZAMIDE AND ITS SALTS 失效制备N-（1,1-二甲基乙基）-4 - [[5'-乙氧基-4- CIS [2-（4-吗啉基）乙氧基] -2'-氧代吡咯并[环己基] -1,3- H]吲哚] 1'（2'-H）-YL] - 磺基] -3-甲氧基苯甲酸及其盐公开(公告)号：US06600039B1
公开(公告)日：2003-07-29
申请号：US10030647
申请日：2002-04-17
申请人： Gergely Héja , Éva Csikós , Tünde Erösné Takácsy , Csaba Gönczi , Judit Halász , István Hermecz , Csilla Majláth , Lajos Nagy , Andrea Sántáné Csutor , Péter Sárosi , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
发明人： Gergely Héja , Éva Csikós , Tünde Erösné Takácsy , Csaba Gönczi , Judit Halász , István Hermecz , Csilla Majláth , Lajos Nagy , Andrea Sántáné Csutor , Péter Sárosi , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07D27300
CPC分类号： C07D209/96
摘要： The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.
摘要翻译： 本发明涉及制备式（I）化合物及其盐的方法，其通过使式（II）化合物与式（III）化合物反应，其包括在二甲基亚砜中进行反应， 温度在10℃至40℃之间，优选在室温下，如果需要，通过本身已知的方法将得到的式（I）碱转化成其盐。
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